Proteolysis Targeting Chimeras (PROTACs) are dual-ended molecules that bind to a target protein and an E3 ligase, and in turn downregulate the target protein via polyubiquitination. Our research consists of the bioanalysis of 8 novel PROTACs in PSN1 pancreatic cancer cells. Each PROTAC consists of an E3 ligase binder, a sphingosine kinase 1 (sk1) inhibitor, and a linker of varying structure and length. In quantitative assays, our PROTACs exhibit a hook effect as expected due to their chimeric nature and our PROTACs have shown to be effective at slowing cell growth at concentrations as low as 20 nM, much lower than the inhibitor alone.

Biological analysis of new PROTACs for downregulation of sphingosine kinase 1

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ACS Spring 2023

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